- RAR-ALPHA COMPOUNDS FOR INFLAMMATORY DISEASE AND MALE CONTRACEPTION
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Modulators of retinoid acid receptor-alpha (RARα) of formula (I) are provided herein, as well as pharmaceutical compositions and methods relating thereto.
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Paragraph 0114
(2021/06/26)
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- POSITRON IMAGING TOMOGRAPHY IMAGING AGENT COMPOSITION AND METHOD FOR DETECTION OF BACTERIAL INFECTION
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This invention provides a composition comprising the compound having the structure: ethyl 2-[19F]F-4-nitrobenzoate, and at least one acceptable carrier. This invention also provides a method of detecting the presence of or location of bacteria
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Page/Page column 41-42
(2021/11/13)
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- RETINOID COMPOUND AND PHARMACEUTICAL COMPOSITION
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PROBLEM TO BE SOLVED: To provide a novel retinoid compound that is low in teratogenicity, and a pharmaceutical composition containing said retinoid compound. SOLUTION: Provided are a retinoid compound which is a compound represented by the following formula (1) or a salt thereof, and a pharmaceutical composition containing said retinoid compound. In the formula, R1 represents a halogen atom, and R2 and R3 each independently represent a silyl group. SELECTED DRAWING: None COPYRIGHT: (C)2020,JPOandINPIT
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Paragraph 0029; 0035
(2020/04/17)
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- Positron Emission Tomography Imaging of Staphylococcus aureus Infection Using a Nitro-Prodrug Analogue of 2-[18F]F- p-Aminobenzoic Acid
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Deep-seated bacterial infections caused by pathogens such as Staphylococcus aureus are difficult to diagnose and treat and are thus a major threat to human health. In previous work we demonstrated that positron emission tomography (PET) imaging with 2-[18
- Daryaee, Fereidoon,Li, Yong,Meimetis, Labros,Noh, Doyoung,Si, Yuanyuan,Smith-Jones, Peter M.,Tonge, Peter J.,Turkman, Nashaat,Walker, Stephen G.,Yoon, Grace E.
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p. 2249 - 2259
(2020/09/21)
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- N-substituted benzenesulfonyl-substituted benzamide compounds and application thereof to drug preparation
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The invention relates toN-substituted benzenesulfonyl-substituted benzamide compounds, crystal forms, pharmaceutically acceptable salts, hydrates, solvates or predrugs of the compounds as well as a preparation method and a pharmaceutical application of th
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Paragraph 0181; 0182; 0183
(2017/09/05)
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- Synthesis and cardiac imaging of 18F-ligands selective for β1-adrenoreceptors
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A series of potent and selective β1-adrenoreceptor ligands were identified (IC50 range, 0.04-0.25 nM; β1/ β2 selectivity range, 65-450-fold), labeled with the PET radioisotope fluorine-18 and evaluated in normal Sprague-Dawley rats. Tissue distribution studies demonstrated uptake of each radiotracers from the blood pool into the myocardium (0.48-0.62% ID/g), lung (0.63-0.97% ID/g), and liver (1.03-1.14% ID/g). Dynamic μPET imaging confirmed the in vivo dissection studies.
- Radeke, Heike S.,Purohit, Ajay,Harris, Thomas D.,Hanson, Kelley,Jones, Reinaldo,Hu, Carol,Yalamanchili, Padmaja,Hayes, Megan,Yu, Ming,Guaraldi, Mary,Kagan, Mikhail,Azure, Michael,Cdebaca, Michael,Robinson, Simon,Casebier, David
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supporting information; experimental part
p. 650 - 655
(2011/11/05)
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- Novel indolyl derivatives which are L-CPT1 inhibitors
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The invention is concerned with novel heterobicyclic derivatives of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, A, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.
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Page/Page column 20-21
(2010/11/26)
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- THERAPEUTIC COMPOUNDS FOR TREATING DYSLIPIDEMIC CONDITIONS
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The present invention relates to novel LXR ligands of Formula (I) and pharmaceutically acceptable salts, esters and tautomers thereof, which are useful in the treatment of dyslipidemic conditions, particularly depressed levels of HDL cholesterol.
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Page/Page column 47-48
(2010/11/28)
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- Novel sulfonamides as L-CPT1 inhibitors
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The invention is concerned with novel sulfonamide derivatives of formula (I) wherein R2, R3, R4, A, X, Y1, Y2, Y3, Y4 and Z1 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.
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Page/Page column 16
(2010/11/25)
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- Therapeutic compounds for treating dyslipidemic conditions
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The present invention relates to novel LXR ligands of Formula I and pharmaceutically acceptable salts, esters and tautomers thereof, which are useful in the treatment of dyslipidemic conditions, particularly depressed levels of HDL cholesterol.
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Page/Page column 29-30
(2008/06/13)
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- New enzymes and prodrugs for ADEPT
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The present invention relates to nucleic acid molecules encoding mutant human carboxypeptidase A enzymes, and encoding conjugates of targeting molecules and mutant human carboxypeptidase A enzymes. The invention further relates to vectors and cell lines containing such nucleic acid molecules.
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- Methods of treatment with compounds having RARα receptor specific or selective activity
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Retinoid compounds which act specifically or selectively on RARα receptor subtypes in preference over RARβ and RARγ receptor subtypes, posses desirable pharmaceutical properties associated with retinoids, and are particularly suitable for treatment of tumors, such as acute monocytic leukemia, cervical carcinoma, myeloma, ovarian carcinomas and head and neck carcinomas, without having one or more undesirable side effects of retinoids, such as inducement of weight loss, mucocutaneous toxicity, skin irritation and teratogenecity.
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- Substituted heteroarylamides having retinoid-like biological activity
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Compounds of the formula STR1 wherein the symbols have the meaning described in the specification, have retinoid-like biological activity.
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- Aryl or heteroaryl amides of tetrahydronaphthalene, chroman, thiochroman and 1,2,3,4,-tetrahydroquinoline carboxylic acids, having an electron withdrawing substituent in the aromatic or heteroaromatic moiety, having retinoid-like biological activity
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Compounds of the formula STR1 where the symbols have the meaning defined in the specification have retinoid-like biological activity.
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- Retinoid-like compounds
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The present invention relates to a compound of formula I STR1 or a nontoxic pharmaceutically acceptable salt, physiologically hydrolyzable ester or solvate thereof, in whichX is --O--CO--, --NH--CO--, --CS--NH--, --CO--O--, --CO--NH--, --COS--, --SCO--, --SCH 2 --, --CH 2 --CH 2 --, --C C--, --CH 2 --NH--, --COCH 2 --, --NHCS--, --CH 2 S--, --CH 2 O--, --OCH 2 --, --NHCH 2 -- or --CR 5 CR 6 --;R m and R k are independently hydrogen, halogen, C 1-6 alkyl, hydroxy, C 1-6 alkyloxy or nitro;n is zero or one;R 4 is --(CH 2) t --Y, C 1-6 alkyl, or C 3-6 cycloalkyl;R 1 is --CO 2 Z, C 1-6 alkyl, CH 2 OH, --CONHR y, or CHO;R 2 and R 3 are independently hydrogen or C 1-6 alkyl;R a and R b are independently hydrogen or C 1-6 alkyl; but when n is one, R a and R b together can form a radical of the formula STR2 Y is naphthyl or phenyl, both radicals can be optionally substituted with one to three same or different C 1-6 alkyl or halogen;Z is hydrogen or C 1-6 alkyl;R 5, R 6 and R y are independently hydrogen or C 1-6 alkyl; andt is zero to six.
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- Retinoid-like compounds
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The present invention relates to a compound of formula STR1 or a nontoxic pharmaceutically acceptable salt, physiologically hydrolyzable ester or solvate thereof, in which X is --O--CO--, --NH--CO--, --CS--NH--, --CO--O--, --CO--NH--, --COS--, --SCO--, --SCH2 --, --CH2 --CH2 --, --C C--, --CH2 --NH--, --COCH2 --, --NHCS--, --CH2 S--, --CH2 O--, --OCH2 --, --NHCH2 -- or --CR5 =CR6 --; Rm and Rk are independently hydrogen, halogen, C1-6 alkyl, hydroxy, C1-6 alkyloxy or nitro; n is zero or one; R4 is --(CH2)t --Y, C1-6 alkyl, or C3-6 cycloalkyl; R1 is --CO2 Z, C1-6 alkyl, CH2 OH, --CONHRy, or CHO; R2 and R3 are independently hydrogen or C1-6 alkyl; Ra and Rb are independently hydrogen or C1-6 alkyl; but when n is one, Ra and Rb together can form a radical of the formula STR2 Y is naphthyl or phenyl, both radicals can be optionally substituted with one to three same or different C1-6 alkyl or halogen; Z is hydrogen or C1-6 alkyl; R5, R6 and Ry are independently hydrogen or C1-6 alkyl; and t is zero to six.
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